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DEVELOPMENT SEQUENCE IN THE SEARCH FOR A MEDICINE The search for a medicine is a long (10-25 years), complex and expensive process consisting of several stages. DRUG PRECLINICAL Launch CLINICAL DEVELOPMENT of the R&D STUDIES(2-10 years) (2-6 years) drug PHASE I  PHASE II  PHASE III In vitro/In vivo PHASE IV

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HOW IS A DRUG CANDIDATE DISCOVERED? • A drug candidate can be discovered in different ways: ?

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HOW IS A DRUG CANDIDATE DISCOVERED?A drug candidate can be discovered in different ways: Serendipity Massive screening chance Chemical modification Rational design

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CLINICAL DEVELOPMENT• Clinical development is the longest and most costly part of the search for new medicines. It consists of three phases: PHASE III PHASE II PHASE I Healthy volunteers Patients (100-300) Patients Safety and (drug or placebo) (1300-3000) dose Efficacy and Long-term side effects effects

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AND FINALLY… THE DRUG IS LAUNCHED ON THE MARKET!• If the drug has successfully passed the three clinical phases, it is launched on the market, but the study continues (Phase IV) PHASE III PHASE II PHASE I PHASE IV

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INTRODUCTION – WHAT IS PARKINSON’S DISEASE?• Parkinson’s disease (PD) is a chronic and progressive movement disorder characterised by: – Coordination problems – Slowed movements – Generalised tremor• It is the second most common neurodegenerative disease and affects 1-2% of people over 60. There are currently more than 4 million people suffering from PD worldwide.

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INTRODUCTION – PARKINSON’S DISEASE, CAUSES• Our brain is our body’s control centre and the cells responsible for it are called neurons. These cells self- regenerate very slowly.• Neurotransmitters are special chemical compounds that enable neurones to “talk to each other” and communicate.

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INTRODUCTION – PARKINSON’S DISEASE, CAUSES• We still do not know what causes Parkinson’s disease, but we do know that it is due to the loss or incorrect functioning of the neurons responsible for producing dopamine, a neurotransmitter. • Dopamine  Control of movement• Dopamine is responsible for transmitting the signals required to control the movement  our muscles. the control Low dopamine levels of Difficulties in of movement• A dopamine deficiency therefore leads to an imbalance in neuronal transmission, preventing neurons from communicating properly. This leads to a loss of motor function.

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INTRODUCTION – PARKINSON’S DISEASE, TREATMENT • The way to treat the disease’s progression is by taking oral medicines. tyrosine L-dopa dopamine vesicles with the dopamine transmitter • The most commonly used medicine today is levodopa, or L-dopa, which consists of a chemical compoundsynapse that the brain uses to produce dopamine.dopaminereceptor receptor cell

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INTRODUCTION – PARKINSON’S DISEASE, TREATMENT• Unfortunately, these medicines have a large number of side effects: – Appearance of involuntary movements and tics – Depression – Hallucinations• These medicines also cease to be effective with time.• We need to produce new medicines with less side effects that are active for longer periods.

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RESEARCH, SYNTHESIS OF DRUGS FOR THE TREATMENT OF PARKINSON’S DISEASE• In the Barcelona Science Park, on the Combinatory Chemistry Platform, scientists are working on the synthesis of new compounds that can be used as therapeutic agents in the treatment of neurodegenerative diseases such as Parkinson’s or Schizophrenia that are: – More active – Less toxic

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RESEARCH, SYNTHESIS OF DRUGS FOR THE TREATMENTOF PARKINSON’S DISEASE • A drug cocktail is currently administered to increase the efficacy of these anti-Parkinson’s agents. • The objective is to synthesise new molecules that are more effective or have less side effects. D AAnti-Parkinson’s agents Drug cocktail A single drug